Pharm

Droperidol

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Droperidol, Inapsine

  • Background
  1. Developed in the 1960s and available in U.S. until 2012, when U.S. manufacturing ceased
    1. Followed 2001 reports of QTc Prolongation
    2. Mayo Clinic continued to use Droperidol between 2001 and 2020 without significant adverse events
  2. Multiple studies demonstrated safety of Droperidol and as of 2015 was cleared to return to market in U.S. (available as of 2019)
  1. Antiemetic in refractory Vomiting
  2. Surgical or Diagnostic procedure
    1. Procedure related Nausea or Vomiting
    2. Conscious Sedation
  3. Migraine Headache
  4. Chemical Restraint (e.g. Sedation of the Violent Patient)
  5. Cannabinoid Hyperemesis
  6. First generation Antipsychotic (Neuroleptic)
  • Contraindications
  1. Absolute contraindications
    1. QT Prolongation prior to use (>440 ms)
  2. Relative contraindications: Risk of QT Prolongation
    1. Congestive Heart Failure
    2. Bradycardia (Heart Rate <50 beats per minute)
    3. Concurrent Diuretic use
    4. Cardiac hypertrophy
    5. Hypokalemia
    6. Hypomagnesemia
    7. Other medication use associated with QT Prolongation
      1. Class I Antiarrhythmics
      2. Class III Antiarrhythmics
      3. Monoamine Oxidase Inhibitors
  • Mechanism
  1. Butyrophenone Neuroleptic (first generation Antipsychotic) similar to Haloperidol
  2. Potent Dopamine receptor antagonist at D2
  3. Serotonin Antagonist activity
  4. Antiemetic activity via Dopamine antagonist
  • Pharmacokinetics
  1. Rapid onset (esp. Droperidol IM compared with Haloperidol IM)
  • Adverse Effects
  1. QT Prolongation
    1. Avoid use with other agents causing Prolonged QT Interval due to Medication
    2. May consider EKG before use (but not required)
    3. FDA Black box warning due to observed QT Prolongation at therepeutic doses
      1. First reported in 2001, but rare in clinical use
      2. Report coincided with release of new, on patent Antiemetic (Ondansetron)
        1. Curiously, 12 years later Ondansetron was reported to have the potential for QTc Prolongation
    4. Studies have since demonstrated its safety when used at moderate dose
      1. Calver (2015) Ann Emerg Med 66(3): 230-8 +PMID:25890395 [PubMed]
      2. Gaw (2020) Am J Emerg Med 38(7): 1310-14 [PubMed]
      3. Jackson (2007) Am J Syst Pharm 64(11): 1174-86 [PubMed]
  2. Sedation
    1. Usually resolves within 4 hours of dose
    2. Alertness may be decreased for 12 hours after dose
  3. Neurologic effects (treat with benztropine, Diphenhydramine)
    1. Extrapyramidal Side Effects
    2. Akasthisia
    3. Dystonia
  4. Neuroleptic Malignant Syndrome
  • Drug Interactions
  1. Other agents that prolong QT Interval (see above)
  1. Adults: 1.25 to 2.5 mg IM or IV slowly (may give up to 5 mg IV or IM)
  2. Children: 0.1 mg/kg IM or IV slowly
  1. Adults: 5 mg IM or slow IV
  1. Adults: 5 mg IM (range 2.5 to 7.5 mg IM) or slow IV
  2. May combine with Midazolam 2 mg (up to 5 mg if needed)
  • Monitoring
  1. Baseline EKG
  2. Continuous cardiac monitoring for 3 hours after dose